Antiestrogenic effects of LY 117018 in MCF-7 cells

S. M. Scholl, K. K. Huff, Marc E Lippman

Research output: Contribution to journalArticle

66 Citations (Scopus)

Abstract

LY 117018 is a nonsteroidal compound which has been shown to antagonize more effectively than tamoxifen the effects of estradiol in rats and mice. We have further defined the properties of this compound on cell growth and progesterone receptor (PR) induction and have compared inhibitory effects to relative binding affinity in a human breast cancer cell line. In MCF-7 cells, LY 117018 [(6-hydroxy-2-(p-hydroxyphenyl)benzo[b]thien-3-yl-p-(2-pyrrolidinyl)ethoxy phenyl ketone] is devoid of estrogenic effects, has a greater affinity for the estrogen receptor (ER) than tamoxifen at 4 C, and is 100-1000 times more potent than tamoxifen at inhibiting cell growth. While tamoxifen has been reported to induce PR, a purported estrogen effect, the LY 117018 compound failed to induce PR using a broad range of concentrations. The direct antagonistic effect of LY 117018 was demonstrated by the use of varying concentrations of LY 117018 and estradiol concomitantly. We conclude that LY 117018 is a very effective antiestrogen devoid of any stimulatory effects among these parameters tested.

Original languageEnglish
Pages (from-to)611-617
Number of pages7
JournalEndocrinology
Volume113
Issue number2
StatePublished - Jan 1 1983
Externally publishedYes

Fingerprint

LY 117018
MCF-7 Cells
Tamoxifen
Progesterone Receptors
Estradiol
Estrogens
Estrogen Receptor Modulators
Growth
Ketones
Estrogen Receptors
Breast Neoplasms
Cell Line

ASJC Scopus subject areas

  • Endocrinology
  • Endocrinology, Diabetes and Metabolism

Cite this

Scholl, S. M., Huff, K. K., & Lippman, M. E. (1983). Antiestrogenic effects of LY 117018 in MCF-7 cells. Endocrinology, 113(2), 611-617.

Antiestrogenic effects of LY 117018 in MCF-7 cells. / Scholl, S. M.; Huff, K. K.; Lippman, Marc E.

In: Endocrinology, Vol. 113, No. 2, 01.01.1983, p. 611-617.

Research output: Contribution to journalArticle

Scholl, SM, Huff, KK & Lippman, ME 1983, 'Antiestrogenic effects of LY 117018 in MCF-7 cells', Endocrinology, vol. 113, no. 2, pp. 611-617.
Scholl SM, Huff KK, Lippman ME. Antiestrogenic effects of LY 117018 in MCF-7 cells. Endocrinology. 1983 Jan 1;113(2):611-617.
Scholl, S. M. ; Huff, K. K. ; Lippman, Marc E. / Antiestrogenic effects of LY 117018 in MCF-7 cells. In: Endocrinology. 1983 ; Vol. 113, No. 2. pp. 611-617.
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